The invention in its broad aspect relates to caprolactam derivatives which are useful as converting enzyme inhibitors and as antihypertensives. The compounds of this invention can be shown by the following formula: ##STR1## wherein R.sup.1 is hydrogen, loweralkyl, cyclic loweralkyl, amino loweralkyl, alkylamino loweralkyl, hydroxyalkyl, acylamino loweralkyl, dialkylamino loweralkyl including cyclic polyethyleneamino loweralkyl, arloweralkyl, aryl, substituted aryl wherein the substituent is halo, alkyl, aminoalkyl, or alkoxy; heteroaryl, heteroarloweralkyl;
R.sup.2 is hydrogen or loweralkyl; PA1 R.sup.3 is hydroxyl, loweralkoxy, or aralkyloxy; PA1 R.sup.4 is hydrogen or loweralkanoyl; and, the pharmaceutically acceptable salts thereof. PA1 alkyl denotes straight and branched hydrocarbons of C.sub.1 -C.sub.12 and loweralkyl denotes straight and branched hydrocarbons of C.sub.1 -C.sub.8 ; PA1 aryl and the prefix "ar" denote unsubstituted aromatic ring or rings of C.sub.6 -C.sub.12 such as, for example, phenyl, naphthyl, biphenyl; PA1 acyl denotes a carboxylic acid derivative represented by the formula ##STR2## wherein R is alkane, aralkane, arene, heteroarene, heteroaralkene, and substituted derivatives thereof so that acyl denotes, for example, alkanoyl, aroyl, aralkanoyl, heteroaryl, heteroaralkanoyl, and the like; PA1 cycloalkyl denotes an unsubstituted alkyl ring of C.sub.3 -C.sub.10 ; PA1 hetero denotes the heteroatoms N, O or S; PA1 heteroaryl denotes an aryl group containing a heteroatom; PA1 heterocycle denotes a saturated or unsaturated aromatic or non-aromatic cyclic compound containing a heteroatom; and PA1 halogen and halo denote F, Br, Cl or I atoms. PA1 R.sup.1 is hydrogen, loweralkyl, aminoloweralkyl, or aryl; PA1 R.sup.2 is hydrogen or loweralkyl; PA1 R.sup.3 is hydroxyl, or loweralkoxy; and, PA1 R.sup.4 is hydrogen or loweralkanoyl.
As used throughout this application, including the claims, and unless specified otherwise:
Preferred are compounds of Formula I wherein
The preferred compounds of this invention also include the pharmaceutically acceptable salts thereof.
The products of Formula (I) and the preferred subgroup can be produced by one or more of the methods and subroutes depicted in the following equations. The definitions of R.sup.1, R.sup.2, R.sup.3 and R.sub.4 are the same as in Formula (I) except where noted.